New potential anti-tumour compounds
Scientists from China have made novel anti-tumour pharmacophores, compounds that carry features responsible for a drug’s biological activity. The team, led by Shiqi Peng, made 20 novel beta-carboline-3-carbonyl-amino acid benzyl esters and investigated their activity as DNA intercalators. DNA intercalation – the inclusion of a molecule between two other molecules – is a pivotal step in the mechanism of many anti-tumor drugs. The discovery of new intercalators could expand possibilities in cancer therapy.
The researchers found that 13 compounds were active against tumours and nine were more active than cytarabine, a compound used to treat acute myeloid leukemia and non-Hodgkin lymphoma. They also carried out toxicity studies and found that the compounds did not damage the immunologic function of mice.
Original publication: L Liu, L Wei, Y Yang, M Zhao, X Zhang, M Zheng, Y Wang and S Peng, MedChemComm, 2011.
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